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OBJECTIVE To study the in vivo pharmacodynamics of paclitaxel-loaded TPGS-modified carboxymethyl chitosan-rhein conjugate micelles (PTX/TPGS-CR micelles) in tumor-bearing mice. METHODS The pH and osmotic pressure value of PTX/TPGS-CR micelles were determined. The 4T1 subcutaneous transplanted tumor model was established in Balb/c mice. Taxol® was used as the positive control, and the tumor growth curve and tumor inhibition rate were used as the main indicators. The safety and efficacy of PTX/TPGS-CR micelles were investigated by observing the changes in body weight, organ index and pathological tissue sections of mice, and measuring the expression of P-gp protein in tumor tissues of each group. RESULTS The pH value was similar to that of 0.9% sodium chloride injection (5.0-7.0), and the osmotic pressure value was 736.6-757.2 kPa. The tumor inhibition rates of Taxol® and PTX/TPGS-CR micelle in low, medium and high dose groups were 29.91%, 20.87%, 41.06% and 41.84%, respectively. The antitumor effect of PTX/TPGS-CR micelles was better than that of Taxol® at the same dose (P<0.05), and showed a dose-dependent feature. During the administration period, the body weight and organ of the mice in the PTX/TPGS-CR micelle group at the same dose showed no significantly affected, indicating that PTX/TPGS-CR micelles had better safety. The results of P-gp expression in tumor tissue showed that TPGS-CR micelles could inhibit the expression of P-gp protein. CONCLUSION PTX/TPGS-CR micelle preparation is a nano preparation with high efficiency and low toxicity. It has a good antitumor effect and can reduce the toxicity of PTX. Moreover, it can improve the sensitivity of tumor cells to PTX by inhibiting the expression of P-gp, which is conducive to the treatment of tumors.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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